Abstract: Substituted indoles of the formula (I) and physiologically acceptable derivatives and salts thereof, in which R1, D, E, R12, p, X1, E, G, X2 and Z are as defined in claim 1, exhibit particular actions on the central nervous system, especially 5HT reuptake-inhibiting and 5 HTx-agonistic and/or -antagonistic actions and in particular serotonin-agonistic and -antagonistic properties and can be employed as antipsychotics, neuroleptics, antidepressants, anxiolytics and/or antihypertonics.
Type:
Application
Filed:
July 29, 2009
Publication date:
November 26, 2009
Inventors:
Oliver SCHADT, Henning Böttcher, Joachim Leibrock, Kai Schiemann, Timo Heinrich, Günter Hölzemann, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
Type:
Application
Filed:
June 21, 2007
Publication date:
November 19, 2009
Inventors:
Marc Capet, Denis Danvy, Nicolas Levoin, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Xavier Ligneau
Abstract: Imidazole-substituted 4-anilino-3-cyanoquinolines are described, which selectively inhibit IFGR kinase activity and are useful for treating disorders associated with IGFR kinases.
Type:
Application
Filed:
April 14, 2009
Publication date:
October 22, 2009
Applicant:
Wyeth
Inventors:
Scott Christian Mayer, Lori Michelle Miller
Abstract: Novel aryl- and heteroarylpiperazines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
Type:
Application
Filed:
February 9, 2009
Publication date:
October 22, 2009
Applicant:
High Point Pharmaceuticals, LLC
Inventors:
Rolf Hohlweg, Florencio Zaragoza Dorwald, Henrik Stephensen, Ingrid Pettersson, Bernd Peschke
Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1, such as obesity, and diabetes.
Type:
Application
Filed:
April 10, 2007
Publication date:
September 24, 2009
Inventors:
Richard Berger, Scott Edmondson, Hansen Alexa, Cheng Zhu
Abstract: Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety. wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description.
Type:
Grant
Filed:
July 2, 2008
Date of Patent:
September 22, 2009
Assignee:
Glaxo Group Limited
Inventors:
Markus Bergauer, Barbara Bertani, Matteo Biagetti, Steven Mark Bromidge, Alessandro Falchi, Colin Philip Leslie, Giancarlo Merlo, Domenica Antonia Pizzi, Marilisa Rinaldi, Luigi Piero Stasi, Jessica Tibasco, Antonio Kuok Keong Vong, Simon Edward Ward
Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
Abstract: The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonistsand are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
Abstract: The present invention provides methods of treating leukemia comprising administration of a resistance modulating amount of a compound having the formula (2r)-anti-5-{3-[4-(10,11-difluoromethano-dibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline 2.5 hydrochloride.
Type:
Grant
Filed:
May 24, 2007
Date of Patent:
September 1, 2009
Assignee:
Eli Lilly and Company
Inventors:
Julie Kay Bush, Susan Marie Reutzel-Edens
Abstract: The invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, R3, Y1, Y2, m, n, W, X, B and Z are defined as cited in claim 1, to medicaments containing said derivatives and to the use of the latter for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases
Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
Abstract: A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based sulfonylhydrazine reactive resin to remove an aldehyde impurity.
Type:
Grant
Filed:
September 12, 2003
Date of Patent:
July 21, 2009
Assignee:
Merck & Co. Inc.
Inventors:
Mirlinda Biba, Paul Compton Collins, Christopher Joseph Welch, David A. Conlon, Antoinette Drahus
Abstract: The present application relates to new compounds of formula (I), to pharmaceutical compositions comprising the compounds, to processes for their preparation, and to the use of the compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.
Type:
Application
Filed:
December 5, 2008
Publication date:
July 9, 2009
Applicant:
Biovitrum AB
Inventors:
Joseph W. Boyd, Giles A. Brown, Michael Higginbottom
Abstract: Use of 1,4-bis(3-aminoalkyl)piperazine derivatives as defined in formula I or II for the manufacture of a pharmaceutical composition intended for the treatment of neurodegenerative diseases, related neurodegenerative diseases, developmental diseases or cancer. The instant invention is also directed to some specific 1,4-bis(3-aminoalkyl)piperazine derivatives and pharmaceutical composition including them.
Type:
Application
Filed:
November 8, 2005
Publication date:
June 11, 2009
Applicants:
UNIVERSITE DU DROIT ET DE LA SANTE- LILLE II, Institut National De La Sante Et De La Recherche Medicale (Inserm)
Inventors:
Nicolas Sergeant, Andre Delacourte, Patricia Melnyk, Luc Buee
Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Type:
Application
Filed:
November 14, 2008
Publication date:
June 4, 2009
Inventors:
SARA S. HADIDA RUAH, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
Abstract: The invention provides compounds of formula (IA), processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
Type:
Application
Filed:
May 2, 2008
Publication date:
June 4, 2009
Inventors:
Richard Evans, Christine Eyssade, Rhonan Ford, Barrie Martin, Toby Thompson, Paul Willis
Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Abstract: The present invention relates to compounds of formula I wherein R1, R2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Type:
Grant
Filed:
November 30, 2005
Date of Patent:
May 5, 2009
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Matthias Heinrich Nettekoven, Olivier Roche, Rosa Maria Rodriguez-Sarmiento
Abstract: The invention relates to compositions and methods for treating nervous disorders. More particularly, the invention relates to methods of treating amyloÊd beta peptide-related disorders, particularly Alzheimer's disease, using Rac1 inhibitors. The invention may be used in mammalian subjects, particularly human subjects, at various stages of the disease, including disease onset. The invention also provides methods of producing, identifying, selecting or optimising compounds for use in the treatment of amyloÊd beta peptide-related disorders, based on a determination of the ability of a test compound to inhibit Rac 1.
Abstract: The present invention relates to novel compounds of the general formula (I) wherein R1, R4, R5 and X are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).
Abstract: 6,7-Dihydro-5H-cyclopenta[b]pyridine and 5,6,7,8-tetrahydroquinoline compounds of Formula (I), including salts, hydrates and solvates thereof, that act as 5-HT2 receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT2c receptors are described herein.
Type:
Grant
Filed:
March 31, 2006
Date of Patent:
March 24, 2009
Assignee:
Pfizer Inc.
Inventors:
Bruce A. Lefker, Kevin K. -C. Liu, Hou Chen, Steven Blair Coffey
Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.
Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hyper-triglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
Type:
Grant
Filed:
March 7, 2005
Date of Patent:
March 17, 2009
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
Abstract: The invention relates to chemical compounds of formula IA or IB: or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
Type:
Application
Filed:
October 13, 2008
Publication date:
February 26, 2009
Applicant:
AstraZeneca AB
Inventors:
Donald Cook, Leslie Dakin, David Del Valle, Thomas Gero, David Scott, Xiaolan Zheng
Abstract: The present invention relates to substituted quinoline hydrazides of Formula (I): wherein R1, R2, R3, R4, R5, X, Y and Z are defined herein, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-2 and/or neurokinin-3 (NK-3) receptors. These compounds can thus be used in methods of treatment to suppress and treat such disorders.
Type:
Application
Filed:
May 5, 2006
Publication date:
February 26, 2009
Inventors:
William Robert Carling, Jason Matthew Elliott, Elena Mezzogori, Michael Geoffrey Neil Russell, Brian John Williams
Abstract: Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and/or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed.
Type:
Application
Filed:
August 21, 2007
Publication date:
February 26, 2009
Inventors:
Aranapakam Mudumbai Venkatesan, Osvaldo Dos Santos, Magda Asselin, George Theodore Grosu, Deborah A. Evrard, Richard Eric Mewshaw, Kristin Meagher
Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1? converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-? inducing factor-(IGIF), or interferon-?-(“IFN-?”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-? production and methods for treating interleukin-1, apoptosis-, and interferon-?-mediated diseases using the compounds and compositions of this invention.
Type:
Application
Filed:
January 22, 2008
Publication date:
February 19, 2009
Inventors:
Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.
Type:
Application
Filed:
August 24, 2005
Publication date:
January 29, 2009
Applicant:
Ferring B.V.
Inventors:
Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
Abstract: The present invention refers to substituted tetrahydro-quinoline-sulfonamide compounds of general formula (I): a method for their preparation, a medicament comprising these compounds and the use of substituted tetrahydro-quinoline-sulfonamide compounds for the preparation of medicaments for 5-HT6 receptor regulation as well as for the treatment of disorders related thereto.
Type:
Application
Filed:
July 18, 2008
Publication date:
January 29, 2009
Applicant:
LABORATORIES DEL DR. ESTEVE, S.A.
Inventors:
Jose Luis Diaz-Fernandez, Ramon Merce-Vidal, Lajos Novak
Abstract: Compounds of formula I in free or salt form, wherein Ar, R1, R2, R3, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.
Abstract: The present invention relates to 2-amino-imidazo[4,5-d]pyridazin-4-ones and 2-amino-imidazo[4,5-c]pyridin-4-ones of general formula wherein R1 to R4 and X are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Grant
Filed:
December 12, 2006
Date of Patent:
January 13, 2009
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Norbert Hauel, Mohammad Tadayyon, Leo Thomas
Abstract: The present invention provides 4-anilino-3-quinolinecarbonitriles compounds useful for treating a subject having an BcrAbl positive leukemia that is resistant to imatinib.
Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, R6, B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Type:
Application
Filed:
May 21, 2008
Publication date:
December 25, 2008
Applicant:
MEMORY PHARMACEUTICALS CORPORATION
Inventors:
Robert Dunn, Truc Minh Nguyen, Wenge Xie, Ashok Tehim
Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Application
Filed:
April 26, 2006
Publication date:
December 18, 2008
Applicant:
Amgen Inc.
Inventors:
Tae-Seong Kim, David Bauer, Steven Bellon, Alessandro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
Abstract: The present invention provides a new anhydrous crystalline form of ciprofloxacin hydrochloride that is substantially free from solvent molecules, and processes of preparation thereof.
Type:
Application
Filed:
May 30, 2007
Publication date:
December 4, 2008
Inventors:
Fabio Eduardo Silva SOUZA, Jan Oudenes, Boris Ivanovich Gorin
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.
Type:
Grant
Filed:
March 16, 2007
Date of Patent:
December 2, 2008
Assignee:
Glaxo Group Limited
Inventors:
Matteo Biagetti, Alessandro Falchi, Colin Philip Leslie, Giancarlo Merlo, Domenica Antonia Pizzi, Marilisa Rinaldi, Luigi Piero Stasi, Jessica Tibasco
Abstract: Disclosed herein are methods of using metaxalone. In one embodiment, the method comprises determining that a patient in need metaxalone therapy is taking a substance that is a n inhibitor or an inducer of a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4, and adjusting administration to the patient of metaxalone or the substance to avoid an adverse event associated with metaxalone. In another embodiment, the method comprises informing a user that metaxalone ais metabolized by a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4. Also included are articles of manufacture comprising a container containing a dosage form of metaxalone, wherein the container is associated with published material informing that metaxalone affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a metaxalone product.
Type:
Application
Filed:
May 28, 2008
Publication date:
November 27, 2008
Applicant:
MUTUAL PHARMACEUTICAL COMPANY, INC.
Inventors:
Richard H. Roberts, Jie Du, Matthew W. Davis
Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
Type:
Application
Filed:
May 21, 2008
Publication date:
November 27, 2008
Inventors:
Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmerman, Andreas P. Termin
Abstract: The present invention relates to compounds of formula I wherein R1, R2, X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
Type:
Grant
Filed:
December 12, 2005
Date of Patent:
November 25, 2008
Assignee:
Hoffman-La Roche Inc.
Inventors:
Matthias Heinrich Nettekoven, Olivier Roche, Rosa Maria Rodriguez-Sarmiento
Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
Type:
Grant
Filed:
May 5, 2006
Date of Patent:
November 25, 2008
Assignee:
Abbott Laboratories
Inventors:
Robert J. Altenbach, Marlon D. Cowart, Huaqing Liu
Abstract: Disclosed herein are urea-based 5-HT receptor modulators, pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and medical use of such compounds for the treatment and/or management of 5-HT receptor-mediated disorders.
Abstract: Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety. wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description.
Type:
Application
Filed:
July 2, 2008
Publication date:
November 13, 2008
Inventors:
Markus Bergauer, Barbara Bertani, Matteo Biagetti, Steven Mark Bromidge, Alessandro Falchi, Colin Philip Leslie, Giancarlo Merlo, Domenica Antonia Pizzi, Marilisa Rinaldi, Luigi Piero Stasi, Jessica Tibasco, Antonio Kuok Keong Vong, Simon Edward Ward
Abstract: Novel substituted azole diones are provided that kill cells, suppress cell proliferation, suppress cell growth, abrogate the cell cycle G2 checkpoint and/or cause adaptation to G2 cell cycle arrest. Methods of making and using the invention compounds are provided. The invention provides substituted azole diones to treat cell proliferation disorders. The invention includes the use of substituted azole diones to selectively kill or suppress cancer cells without additional anti-cancer treatment. The invention includes the use of cell cycle G2-checkpoint-abrogating substituted azole diones to selectively sensitize cancer cells to DNA damaging reagents, treatments and/or other types of anti-cancer reagents.
Abstract: The present invention relates to novel metabolites of 5-Fluoro-8-{4-[4-(6-methoxyquinolin-8-yl)piperazin-1-yl]piperidin-1-yl}quinoline, which can be useful in treating CNS disorders. The present invention further relates to processes for their preparation, to pharmaceutical compositions comprising them, and to methods of using them.
Type:
Application
Filed:
November 27, 2007
Publication date:
October 23, 2008
Applicant:
Wyeth
Inventors:
Jianyao Wang, Alana Upthagrove, Lin Deng, Wayne Everett Childers, Zhongqi Shen, William Demaio, Robin D. Moore, Zeen Tong, Li Shen, Pixu Li, Michael K. May
Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
Type:
Application
Filed:
July 21, 2006
Publication date:
October 23, 2008
Applicant:
ChemoCentryx, Inc.
Inventors:
Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
Abstract: Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other disorders.
Type:
Grant
Filed:
September 23, 2004
Date of Patent:
October 21, 2008
Assignee:
Glaxo Group Limited
Inventors:
Christopher Norbert Johnson, Stephen Frederick Moss, David R Witty
Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of thiazolidinedione derivatives.
Type:
Application
Filed:
August 24, 2007
Publication date:
October 16, 2008
Inventors:
Michael Gerard Darcy, Steven David Knight, Nicholas D. Adams, Stanley J. Schmidt